Which medications in the drug class Tyrosine kinase inhibitors and VEGF inhibitors are used in the treatment of Renal Cell Carcinoma?

Updated: May 21, 2019
  • Author: Kush Sachdeva, MD; Chief Editor: E Jason Abel, MD  more...
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Answer

Tyrosine kinase inhibitors and VEGF inhibitors

Sorafenib (Nexavar)

Sorafenib is indicated for advanced renal cell carcinoma. This agent was the first oral multikinase inhibitor that targeted serine/threonine and tyrosine receptor kinases in both the tumor cell and the tumor vasculature. Sorafenib targets kinases involved in tumor cell proliferation and angiogenesis, thereby decreasing tumor cell proliferation. These kinases included RAF kinase, vascular endothelial growth factor receptor (VEGFR)-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-beta, stem cell factor receptor (KIT), and Fmslike tyrosine kinase-3 (FLT-3).

Axitinib (Inlyta)

Axitinib inhibits receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3. It is indicated for treatment of advanced renal cell carcinoma after failure of 1 prior systemic therapy.

Sunitinib (Sutent)

Sunitinib is a multikinase inhibitor that targets several tyrosine kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression. This agent inhibits PDGFRs (ie, PDGFR-alpha, PDGFR-beta), VEGFRs (ie, VEGFR1, VEGFR2, VEGFR3), KIT, FLT3, colony-stimulating factor receptor type 1 (CSF-1R), and the glial cell-line–derived neurotrophic factor receptor (RET).

Pazopanib (Votrient)

Pazopanib is a multityrosine kinase inhibitor indicated for advanced renal cell carcinoma. This agent selectively inhibits VEGFR-1, -2 and -3, c-kit, and PDGFR, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated. [58]

Lenvatinib (Lenvima)

Tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors for VEGFR-1, -2, -3, FGFR -1, -2, -3, and -4, PDGFR-alpha, KIT and RET pathways. The combination of everolimus and lenvatinib shows increased ant-angiogenesis properties.  The combination is indicated for advanced renal cell carcinoma in patients who have received prior antiangiogenic therapy. It is indicated for advanced RCC in combination with everolimus following 1 prior antiangiogenic therapy.

Cabozantinib (Cabometyx)

Tyrosine kinase inhibitor that targets RET, MET, VEGFR-1, -2, and -3, KIT, TrkB, FLT-3, AXL, and TIE-2 pathways. It is indicated for advanced renal cell carcinoma.

Bevacizumab (Avastin, Mvasi)

Bevacizumab is a recombinant, humanized monoclonal antibody that inhibits angiogenesis by targeting and inhibiting VEGF. Bevacizumab is indicated for the treatment of metastatic kidney cancer in combination with interferon alfa. Mvasi has been FDA-approved as a biosimilar to Avastin but not as an interchangeable product.


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